EP2457908B8 - Process for the Preparation of Compounds useful as inhibitors of SGLT - Google Patents
Process for the Preparation of Compounds useful as inhibitors of SGLT Download PDFInfo
- Publication number
- EP2457908B8 EP2457908B8 EP12156039.5A EP12156039A EP2457908B8 EP 2457908 B8 EP2457908 B8 EP 2457908B8 EP 12156039 A EP12156039 A EP 12156039A EP 2457908 B8 EP2457908 B8 EP 2457908B8
- Authority
- EP
- European Patent Office
- Prior art keywords
- sglt
- inhibitors
- preparation
- compounds useful
- compounds
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
- C07D333/12—Radicals substituted by halogen atoms or nitro or nitroso radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
- C07H13/02—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
- C07H13/04—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals attached to acyclic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
- C07H7/04—Carbocyclic radicals
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Diabetes (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Emergency Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Saccharide Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Priority Applications (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SM20170092T SMT201700092T1 (en) | 2008-10-17 | 2009-10-15 | Process for the preparation of compounds useful as inhibitors of sglt |
| SI200931615A SI2457908T1 (en) | 2008-10-17 | 2009-10-15 | Process for the Preparation of Compounds useful as inhibitors of SGLT |
| PL12156039T PL2457908T3 (en) | 2008-10-17 | 2009-10-15 | Process for the Preparation of Compounds useful as inhibitors of SGLT |
| RS20170048A RS55577B1 (en) | 2008-10-17 | 2009-10-15 | METHOD OF PREPARING UNITS USEFUL AS USEFUL SLGT INHIBITORS |
| HRP20170255TT HRP20170255T1 (en) | 2008-10-17 | 2017-02-17 | Process for the preparation of compounds useful as inhibitors of sglt |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10626008P | 2008-10-17 | 2008-10-17 | |
| US10623108P | 2008-10-17 | 2008-10-17 | |
| US12/578,934 US9056850B2 (en) | 2008-10-17 | 2009-10-14 | Process for the preparation of compounds useful as inhibitors of SGLT |
| EP09736928A EP2346888B1 (en) | 2008-10-17 | 2009-10-15 | Process for the preparation of compounds useful as inhibitors of sglt |
Related Parent Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP09736928.4 Division | 2009-10-15 | ||
| EP09736928A Division EP2346888B1 (en) | 2008-10-17 | 2009-10-15 | Process for the preparation of compounds useful as inhibitors of sglt |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| EP2457908A1 EP2457908A1 (en) | 2012-05-30 |
| EP2457908B1 EP2457908B1 (en) | 2016-11-23 |
| EP2457908B8 true EP2457908B8 (en) | 2017-04-05 |
Family
ID=42106967
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP09736928A Active EP2346888B1 (en) | 2008-10-17 | 2009-10-15 | Process for the preparation of compounds useful as inhibitors of sglt |
| EP12156035.3A Active EP2455374B1 (en) | 2008-10-17 | 2009-10-15 | Process for the Preparation of Compounds useful as inhibitors of SGLT |
| EP12156039.5A Active EP2457908B8 (en) | 2008-10-17 | 2009-10-15 | Process for the Preparation of Compounds useful as inhibitors of SGLT |
Family Applications Before (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EP09736928A Active EP2346888B1 (en) | 2008-10-17 | 2009-10-15 | Process for the preparation of compounds useful as inhibitors of sglt |
| EP12156035.3A Active EP2455374B1 (en) | 2008-10-17 | 2009-10-15 | Process for the Preparation of Compounds useful as inhibitors of SGLT |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US9056850B2 (en) |
| EP (3) | EP2346888B1 (en) |
| JP (3) | JP6123111B2 (en) |
| KR (2) | KR101679593B1 (en) |
| CN (3) | CN103467439B (en) |
| AR (1) | AR073892A1 (en) |
| AU (1) | AU2009305413B2 (en) |
| BR (1) | BRPI0920356B1 (en) |
| CA (2) | CA2740853C (en) |
| CL (1) | CL2011000849A1 (en) |
| CY (3) | CY1113867T1 (en) |
| DK (3) | DK2457908T3 (en) |
| EA (1) | EA021373B1 (en) |
| ES (3) | ES2611881T3 (en) |
| HK (1) | HK1224289A1 (en) |
| HR (3) | HRP20130254T1 (en) |
| HU (2) | HUE052432T2 (en) |
| IL (2) | IL212270A0 (en) |
| LT (2) | LT2455374T (en) |
| MX (1) | MX2011004054A (en) |
| NZ (1) | NZ592204A (en) |
| PL (3) | PL2457908T3 (en) |
| PT (3) | PT2457908T (en) |
| RS (3) | RS55577B1 (en) |
| SI (3) | SI2457908T1 (en) |
| SM (4) | SMT201700092T1 (en) |
| TW (3) | TWI588143B (en) |
| UA (1) | UA107450C2 (en) |
| WO (1) | WO2010043682A2 (en) |
| ZA (1) | ZA201103587B (en) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101801371B (en) * | 2007-09-10 | 2012-11-28 | 詹森药业有限公司 | Process for the preparation of compounds useful as SGLT inhibitors |
| US9056850B2 (en) * | 2008-10-17 | 2015-06-16 | Janssen Pharmaceutica N.V. | Process for the preparation of compounds useful as inhibitors of SGLT |
| US20110009347A1 (en) | 2009-07-08 | 2011-01-13 | Yin Liang | Combination therapy for the treatment of diabetes |
| KR101532412B1 (en) | 2009-07-10 | 2015-06-29 | 얀센 파마슈티카 엔.브이. | Crystallization method of 1- (β-D-glucopyranosyl) -4-methyl-3- (5- (4-fluorophenyl) -2-thienylmethyl) benzene |
| SG10201500258WA (en) * | 2009-10-14 | 2015-03-30 | Janssen Pharmaceutica Nv | Process for the preparation of compounds useful as inhibitors of sglt2 |
| US8163704B2 (en) | 2009-10-20 | 2012-04-24 | Novartis Ag | Glycoside derivatives and uses thereof |
| LT2568988T (en) * | 2010-05-11 | 2016-09-12 | Janssen Pharmaceutica, N.V. | Pharmaceutical formulations comprising 1-(beta-d-glucopyranosyl)-2-thienylmethylbenzene derivatives as inhibitors of sglt |
| CN102970981A (en) * | 2010-07-06 | 2013-03-13 | 詹森药业有限公司 | Formulation for co-therapy treatment of diabetes |
| AU2012241897C1 (en) * | 2011-04-13 | 2017-05-11 | Janssen Pharmaceutica Nv | Process for the preparation of compounds useful as inhibitors of SGLT2 |
| TWI542596B (en) | 2011-05-09 | 2016-07-21 | 健生藥品公司 | (2S,3R,4R,5S,6R)-2-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-6-(hydroxyl L-proline and citric acid cocrystals of methyl)tetrahydro-2H-piperan-3,4,5-triol |
| WO2013152476A1 (en) | 2012-04-10 | 2013-10-17 | Theracos, Inc. | Process for the preparation of benzylbenzene sglt2 inhibitors |
| US10323056B2 (en) | 2013-05-08 | 2019-06-18 | Lek Pharmaceuticals D.D. | Crystalline hydrates of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene |
| CN104418834B (en) * | 2013-08-23 | 2017-09-15 | 重庆博腾制药科技股份有限公司 | A kind of synthetic method of antidiabetic medicine intermediate |
| CN104418847A (en) * | 2013-09-10 | 2015-03-18 | 天津药物研究院 | Process for preparing 4-(6-deoxidized-beta-D-glucopyranose)-2-[5-(4-fluorophenyl) thiophene-2-methyl]-1-methyl benzol |
| CN103601715B (en) * | 2013-11-22 | 2015-08-19 | 沈阳化工大学 | A kind of separating and purifying method of 2-(4-fluorophenyl) thiophene |
| EP2918579A1 (en) | 2014-03-14 | 2015-09-16 | LEK Pharmaceuticals d.d. | Synthesis of 2-arylmethyl-5-aryl-thiophene |
| EP2933255A1 (en) | 2014-04-17 | 2015-10-21 | LEK Pharmaceuticals d.d. | Novel crystalline form of 1-(beta-D-glucopyranosyl)-4- methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene |
| ES2711804T3 (en) | 2014-05-27 | 2019-05-07 | Glenmark Pharmaceuticals Ltd | Process for the preparation of canagliflozin |
| CN105330706B (en) * | 2014-06-05 | 2019-04-16 | 江苏豪森药业集团有限公司 | The preparation method of canagliflozin intermediate |
| CN104119324B (en) * | 2014-07-23 | 2016-03-30 | 齐鲁天和惠世制药有限公司 | A kind of preparation method of canagliflozin |
| CN104292209A (en) * | 2014-09-11 | 2015-01-21 | 浙江丽晶化学有限公司 | Novel method for preparing 2-(4-fluorophenyl) thiophene (compound V) |
| CN104402946B (en) * | 2014-11-17 | 2018-01-02 | 连云港恒运药业有限公司 | Canagliflozin intermediate and its unbodied preparation method |
| WO2016083790A1 (en) * | 2014-11-25 | 2016-06-02 | Cipla Limited | Process for the preparation of canagliflozin |
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| WO2018207111A1 (en) | 2017-05-09 | 2018-11-15 | Piramal Enterprises Limited | A process for the preparation of sglt2 inhibitors and intermediates thereof |
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